KR20110047280A - Oral Compositions for the Treatment of Cellulite - Google Patents

Oral Compositions for the Treatment of Cellulite Download PDF

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Publication number
KR20110047280A
KR20110047280A KR1020117009257A KR20117009257A KR20110047280A KR 20110047280 A KR20110047280 A KR 20110047280A KR 1020117009257 A KR1020117009257 A KR 1020117009257A KR 20117009257 A KR20117009257 A KR 20117009257A KR 20110047280 A KR20110047280 A KR 20110047280A
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cellulite
phospholipids
complex
asiatica
treatment
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KR1020117009257A
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Korean (ko)
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에지오 봄바르델리
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인데나 에스피아
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/16Ginkgophyta, e.g. Ginkgoaceae (Ginkgo family)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/23Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/87Vitaceae or Ampelidaceae (Vine or Grape family), e.g. wine grapes, muscadine or peppervine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Abstract

본 발명은 포도(Vitis vinifera) 추출물, 은행(Ginkgo biloba) 후라보노이드류 이량체 및 센텔라 아시아티카(Centella asiatica) 트리텔펜류의 유리형태 또는 인지질과의 착체를 포함하는 셀룰라이트(cellulite) 치료작용을 갖는 경구용 약제 및 화장품 조성물에 관한 것이다.The present invention is grape ( Vitis vinifera extract, Ginkgo biloba ) Flavonoid dimer and Centella asiatica asiatica ) relates to oral pharmaceutical and cosmetic compositions having a cellulite therapeutic action comprising a complex of tritelpenes with free or phospholipids.

Description

셀룰라이트의 치료를 위한 경구용 조성물{Oral compositions for the treatment of cellulite}Oral compositions for the treatment of cellulite

본 발명은 셀룰라이트(cellulite)의 치료를 위한 식물 기원의 성분을 함유한 약제 및 화장품 조성물에 관한 것이다.The present invention relates to pharmaceutical and cosmetic compositions containing ingredients of plant origin for the treatment of cellulite.

보다 상세하게, 본 발명은 포도(Vitis vinifera extracts) 추출물, 은행(Ginkgo biloba) 후라보노이드류 이량체, 그리고 센텔라 아시아티카(Centella asiatica) 트리텔펜류와 같은 활성 성분을 함유한 셀룰라이트(cellulite) 치료를 위한 약제 및 화장품 경구 조성물에 관한 것이다.
More specifically, the present invention is grape ( Vitis vinifera extracts extract, Ginkgo biloba ) flavonoids dimer, and pharmaceutical and cosmetic oral compositions for the treatment of cellulite containing active ingredients such as Centella asiatica tritelpenes.

셀룰라이트(cellulite)는 서구 인구의, 특히 여성에 있어서, 비만에 걸리지 않은 보통 신체 체중의 많은 성인 여성을 포함하여 주목할만한 증가 퍼센트에 영향이 있다. 셀룰라이트는 지방층병변(panniculopathy) 상태와 연관이 있고, 부족한 말초 순환(peripheral circulation), 부종(oedema), 섬유증(fibrosis)과 변화된 지방세포 물질대사의 특징이 있으며, 이상적인 치료는 모든 이들 양상을 고려해야 한다.
Cellulite affects a noticeable increase in the western population, especially in women, including many adult women of normal body weight who are not obese. Cellulite is associated with a panniculopathy condition, characterized by poor peripheral circulation, oedema, fibrosis and altered fat cell metabolism, and ideal treatment should consider all these aspects. do.

셀룰라이트 치료용 경구용 조성물을 제공하기 위함이다.
It is to provide an oral composition for treating cellulite.

[발명의 상세한 설명]Detailed description of the invention

본 발명에 따르면, 활성 성분은 유리형(free form) 또는 인지질(phospholipids)과 착체를 이루고 있다.According to the invention, the active ingredient is complexed with free form or phospholipids.

셀룰라이트(cellulite)는 서구 인구의, 특히 여성에 있어서, 비만에 걸리지 않은 보통 신체 체중의 많은 성인 여성을 포함하여 주목할만한 증가 퍼센트에 영향이 있다. 셀룰라이트는 지방층병변(panniculopathy) 상태와 연관이 있고, 부족한 말초 순환(peripheral circulation), 부종(oedema), 섬유증(fibrosis)과 변화된 지방세포 물질대사의 특징이 있으며, 이상적인 치료는 모든 이들 양상을 고려해야 한다.Cellulite affects a noticeable increase in the western population, especially in women, including many adult women of normal body weight who are not obese. Cellulite is associated with a panniculopathy condition, characterized by poor peripheral circulation, oedema, fibrosis and altered fat cell metabolism, and ideal treatment should consider all these aspects. do.

셀룰라이트의 치료를 위한 많은 약제 및 화장품 조성물은 시장에서 즉시 입수가능하다 : 식물 기원의 예를 들어, 담쟁이덩쿨(ivy), 마로니에(horse-chestmut) 또는 콜라 트리(kola tree)(Centella asiatica) 추출물, 카페인(caffeine), 베타아드레날린성 흥분제(beta-adrenergic stimulants), 메틸잔틴(methylxanthines) 그리고 이와 같은 활성 성분들에 일반적으로 기초화된 것이다. 그러나, 진실로 효과가 입증된 것은 없고, 종종 식이요법에 기인한 개선이 있을지라도 그들 자신의 조성물 용도보다는 조성물의 용도와 관련된 것이었다.Many pharmaceutical and cosmetic compositions for the treatment of cellulite are readily available on the market: for example of plant origin, extracts of ivy, horse-chestmut or kola tree (Centella asiatica) Caffeine, beta-adrenergic stimulants, methylxanthines, and the like based on these active ingredients. However, nothing really has been proven effective, and often associated with the use of the composition rather than their own use, even with improvements due to diet.

식물기원의 활성 성분의 합제를 함유한 경구용 약제 및/또는 화장품 조성물은, 본 발명의 목적하는, 셀룰라이트의 치료, 피하지방의 축적과 "오렌지 껍질" 피부의 뚜렷한 감소에 최선의 결과를 주는 것이고, 고맙게도 다양한 성분의 다른 활성의 합제를 이루며, 항부종(antioedema), 항포스포디에스테라시스(antiphosphodiesterasis), 바소키네틱(vasokinetic) 활성을 발휘하고 콜라겐 생성을 촉진한다. 발명의 조성물은 하지 정맥부전증(venous insufficiency of the lower limbs)의 치료에 효과적이라는 것 역시 증명되었다.Oral pharmaceutical and / or cosmetic compositions containing a combination of plant-derived active ingredients give the best results for the treatment of cellulite, the accumulation of subcutaneous fat and a marked reduction in the "orange peel" skin of the present invention. Thankfully, it combines different activities of various components, exerts antioedema, antiphosphodiesterasis, vasokinetic activity and promotes collagen production. The compositions of the invention have also been demonstrated to be effective in the treatment of venous insufficiency of the lower limbs.

본 발명의 조성물의 모든 활성 성분은 알려져 있고, 약제 및/또는 화장품에 사용된다 ; 그러나 조성물은 상승 효과를 보여주고, 각각 사용된 단일 활동의 활성은 합제로 사용된 활성의 것보다 훨씬 낮다는 것에 주목해야 한다.All active ingredients of the compositions of the invention are known and used in medicaments and / or cosmetics; However, it should be noted that the compositions show a synergistic effect and that the activity of each single activity used is much lower than that of the combination used.

본 발명의 조성물은 포도(Vitis vinifera) 추출물을 용량단위(unit dose) 당 10 내지 500 mg, 은행(Ginkgo biloba) 후라보노이드류 이량체 10 내지 500 mg 및 센텔라 아시아티카(Centella asiatica) 10 내지 500 mg 또는 대응하는 인지질착체의 균등량을 포함할 수 있다.
The composition of the present invention is grape ( Vitis vinifera extract from 10 to 500 mg per unit dose, Ginkgo biloba ) flavonoid dimer 10 to 500 mg and Centella asiatica asiatica ) 10 to 500 mg or an equivalent amount of the corresponding phospholipid complex.

성분 a) - c) 의 유리형태는 상업적으로 유용하다.The free form of components a) -c) is commercially available.

포도(Vitis vinifera) 추출물의 인지질 착체(이하 "성분 a"라 한다)는 유럽특허 제275,224호에 기재되어 있다. 이 추출물은 포도(Vitis vinifera) 종자 중에 포함된 폴리페놀 분획으로 구성되며, 갈릭산(gallic acid), 카테친(catechin) 및 에피카테친(epicatechin) 단량체, 이량체, 삼량체, 사량체, 오량체, 육량체 및 칠량체를 유리형태 또는 갈릭산과의 에스텔 형태로 포함한다. Vitis Phospholipid complexes of vinifera ) extracts (hereinafter referred to as "component a") are described in EP 275,224. The extract is grapes ( Vitis vinifera ), consisting of polyphenol fractions contained in seeds, containing gallic acid, catechin and epicatechin monomers, dimers, trimers, tetramers, pentamers, hexamers and hepters In free form or in ester form with gallic acid.

시험관내 또는 생체실험에서 추출물의 높은 항산화제능력을 보였으며(실험모델에 의존적으로, 비타민 E의 항산화능 보다 10 내지 200 배 이상 높았다), 대부분의 반응선 기종(radical species)을 제거할 수 있었고, 유해효능에 반작용을 보였다. 더욱이 추출물은 잔틴-옥시다제(xanthine-oxidase)와 킬레이트 Cu++ 및Fe+++를 억제할 수 있으며, 따라서, 조직 중 유리라디칼의 효소 촉매적 생산을 예방할 수 있었다. 마지막으로, 포도(Vinis vinifera) 추출물은 콜라게나제(collagenase) 및 다른 푸로테아제(proteases)를 억제하며, 그로 인해 UV 자극에 따른 단백질 분해효소의 유해작용으로부터, 그리고 피부의 염증반응 과정 중에서 연조직 및 피부를 보호하고 ; 더욱이 추출물은 피부 및, 미세혈관 및 모세혈관과 같은 순환구조물에 대하여 선택적 친화력을 갖으며, 따라서, 순환기계에 대한 보호작용 역시 한다.In vitro or in vivo experiments showed a high antioxidant capacity of the extract (depending on the experimental model, 10 to 200 times higher than the antioxidant capacity of vitamin E), was able to remove most of the radical species It has a negative effect on the harmful effects. Moreover, the extract could inhibit xanthine-oxidase and chelate Cu ++ and Fe +++ , thus preventing the enzymatic catalytic production of free radicals in tissues. Finally, grapes ( Vinis vinifera ) extracts inhibit collagenase and other proteases, thereby protecting soft tissues and skin from the harmful effects of proteolytic enzymes upon UV stimulation and during the inflammatory process of the skin; Moreover, the extract has a selective affinity for skin and circulatory structures such as microvessels and capillaries, thus also protecting the circulatory system.

은행(Ginkgo biloba) 후라보노이드류 이량체와 인지질과의 착체(이하, "성분 b"라 한다)은, 유럽 특허 제0275005호에 기재되어 있으며, 은행(Ginko biloba) 후라본류 이량체의 유리형태와 동일한 효력을 갖지만, 활성물질의 더 큰 지속방출을 유도하며, 생물학적 활성(bioavailablity)이 더 우수하다. 은행(Ginkgo biloba) 후라보노이드류 이량체는 특히 비만세포(mast cells)로부터 히스타민과 cAMP 포스포디에스테라제의 방출을 억제한다는 점에서 혈관작용제로서 효능이 있다. 특히, cAMP 포스포디에스테라제의 억제는 cAMP 수치를 증가시키고 ; cAMP는 지방세포(lipocytes)대사를 활성화시키기 때문에 이들 착체화합물은 지질분해작용을 하고 미세혈관관류(microvascular perfusion) 및 피부영양(cutaneous trophism)을 개선시킨다.Bank ( Ginkgo biloba ) complexes of flavonoid dimers and phospholipids (hereinafter referred to as "component b") are described in European Patent No. 0275005, Ginko biloba ) has the same potency as the free form of flavonoid dimers, but induces greater sustained release of the active substance and better bioavailablity. Bank ( Ginkgo biloba ) Flavonoid dimers are particularly effective as vascular agents in that they inhibit the release of histamine and cAMP phosphodiesterase from mast cells. In particular, inhibition of cAMP phosphodiesterase increases cAMP levels; Because cAMP activates lipocyte metabolism, these complexes act to lipolyse and improve microvascular perfusion and cutaneous trophism.

센텔라 아시아티카(Centella asiatica) 추출물의 인지질 착체(이하 "성분 c"라 한다)는 유럽 특허 제0283713호에 기재되어 있다. 이 추출물은 콜라겐 대사에 높은 활성을 보이는 3개의 상이한 분자물의 4 : 3 : 3 혼합물로 구성되며 ; 아시아티코사이드(asiaticoside), 아시아틱산(asiatic acid) 및 마데카식산(madecassic acid)으로 구성되어 있다. 이들 분자물들은 아미노산, 주로 엘-푸로린(L-proline)과 엘-하이드록시푸로린(L-hydroxyproline)의 섬유아세포(fibroblasts)의 소비를 개선시켰으며, 이들 아미노산은 양과 질 모든 면에서 콜라겐 구조 중 가장 중요한 아미노산이다. 개선된 콜라겐 생합성은 퇴화된 노화섬유를 새섬유로 빠른 대체를 일으키게 한다. Centella asiatica phospholipid complexes (hereinafter referred to as "component c") of asiatica ) extracts are described in European Patent No. 0283713. This extract consists of a 4: 3: 3 mixture of three different molecular molecules that show high activity in collagen metabolism; It is composed of asiaticoside, asiatic acid and madecassic acid. These molecules have improved the consumption of fibroblasts of amino acids, mainly L-proline and L-hydroxyproline, and these amino acids have collagen structures in both quantity and quality. Among the most important amino acids. Improved collagen biosynthesis causes rapid replacement of degraded aging fibers with new fibers.

본 발명에 따른 조성물은, 적당한 제형으로 경구적으로 투여되며, 액상제제(시럽, 용액, 현탁제 등) 또는 고형제제(정제, 슈가코팅된 환제, 캅셀제, 저작정 등)등이 있다. 이들 제제는 "레밍톤 파마슈티칼 핸드북"(Remington's Pharmaceutical Handbook), Mack Publishing Co., NY, USA 에 기재된 관용의 방법으로 적당한 부형제를 사용하여 제조될 수 있다.
The composition according to the present invention is administered orally in a suitable formulation, and may include liquid preparations (syrups, solutions, suspensions, etc.) or solid preparations (tablets, sugar-coated pills, capsules, chewable tablets, etc.). These formulations can be prepared using suitable excipients by the conventional methods described in "Remington's Pharmaceutical Handbook", Mack Publishing Co., NY, USA.

본 발명에 따르면 셀룰라이트 치료용 식물기원의 경구용 약제 및 화장품 조성물을 얻을 수 있다는 특장점이 있다.According to the present invention has the advantage that it can obtain oral pharmaceutical and cosmetic compositions of plant origin for cellulite treatment.

본 발명에 따른 조성물의 실시예를 하기에 기재하였다.
Examples of compositions according to the invention are described below.

[실시예][Example]

실시예 1 : 정제 Example 1 : Tablet

포도(Vitis vinifera) 추출물의 인지질 착체 240 mg Vitis vinifera ) 240 mg phospholipid complex

은행(Ginko biloba) 후라보노이드류 이량체의 인지질 착체 100 mgBank ( Ginko biloba ) Phospholipid complex of flavonoid dimer 100 mg

센텔라 아시아티카(Centella asiatica) 트리텔펜류의 Centella asiatica asiatica ) tritelene

인지질 착체 60 mgPhospholipid Complex 60 mg

소디움 클로스카라멜로스 28 mgSodium Clos Caramelose 28 mg

실리콘 디옥사이노 8 mgSilicon Dioxino 8 mg

탈크 4 mg
Talc 4 mg

실시예Example 2 2 : :

포도(Vitis vinifera) 추출물 150 mg Vitis vinifera extract 150 mg

은행(Ginko biloba) 후라보노이드류 이량체 100 mgBank ( Ginko biloba ) flavonoid dimer 100 mg

센텔라 아시아티카(Centella asiatica) 트리텔펜류 10 mg Centella asiatica asiatica ) Tritelenes 10 mg

디칼슘포스페이트 이수화물 150 mgDicalcium phosphate dihydrate 150 mg

미결정 셀룰로스 100 mg100 mg of microcrystalline cellulose

클로스 카라멜로스 소디움 28 mgClos Caramelose Sodium 28 mg

실리콘 디옥사이드 8 mgSilicon dioxide 8 mg

마그네슘 스테아레이트 9 mgMagnesium Stearate 9 mg

탈크 3 mgTalc 3 mg

Claims (4)

a) 포도(Vitis vinifera) 추출물 또는 그의 인지질과의 착체 ;
b) 은행(Ginkgo biloba) 후라보노이드류 이량체 또는 그의 인지질과의 착체 ;
c) 센텔라 아시아티카(Centella asiatica) 또는 그의 인지질과의 착체,
와 관용의 부형제 및 담체를 혼합물 중에 포함한 셀룰라이트(cellulite) 치료용 경구용 약제 조성물.
a) Vitis vinifera ) extract or its complex with phospholipids;
b) Ginkgo biloba) flavonoid complexes of acids and dimer or a phospholipid;
c) Centella Asiatica asiatica ) or its complex with phospholipids,
Oral pharmaceutical composition for treating cellulite, comprising a conventional excipient and a carrier in a mixture.
청구항 1에 있어서, a) - c)의 성분들이 유리형태(free form)인 조성물.The composition of claim 1, wherein the components of a) -c) are in free form. 청구항 1에 있어서, a) - c)의 성분들이 인지질과의 착체 형태인 조성물.The composition of claim 1, wherein the components of a) -c) are in complex form with phospholipids. a) 포도(Vitis vinifera) 추출물 또는 그의 인지질과의 착체 ;
b) 은행(Ginkgo biloba) 후라보노이드류 이량체 또는 그의 인지질과의 착체 ;
c) 센텔라 아시아티카(Centella asiatica) 또는 그의 인지질과의 착체를,
포함하는 하지(lower limbs) 정맥부전증(venous insufficiency) 치료용 경구용 약제 조성물.
a) Vitis vinifera ) extract or its complex with phospholipids;
b) Ginkgo biloba) flavonoid complexes of acids and dimer or a phospholipid;
c) Centella Asiatica asiatica ) or its complex with phospholipids,
Oral pharmaceutical composition for the treatment of lower limbs venous insufficiency.
KR1020117009257A 2003-09-19 2004-09-10 Oral Compositions for the Treatment of Cellulite KR20110047280A (en)

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IT001789A ITMI20031789A1 (en) 2003-09-19 2003-09-19 PHARMACEUTICAL AND COSMETIC COMPOSITIONS FOR TREATMENT
PCT/EP2004/010148 WO2005027947A1 (en) 2003-09-19 2004-09-10 Oral compositions for the treatment of cellulite

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CN104906153A (en) * 2015-06-09 2015-09-16 邳州鑫源生物制品有限公司 Technological method for efficiently extracting ginkgo flavone
CN104940253A (en) * 2015-06-29 2015-09-30 兰捷 Method for extracting high-purity total flavonoids from ginkgo leaves
KR20200115927A (en) * 2019-03-29 2020-10-08 주식회사 유니베라 Composition containing grape leaf extract and centella asiatica extract for improvement of venous circulation disorder

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